1037798-41-6
1037798-41-6 結(jié)構(gòu)式
基本信息
中文別名
化合物 T12650 英文別名
R916562R916562,R-916562
1H-1,2,4-Triazole-3,5-diamine, N3-[4-[4-(1R,2R,4S)-bicyclo[2.2.1]hept-2-yl-1-piperazinyl]phenyl]-1-(2-chloro-7-methylthieno[3,2-d]pyrimidin-4-yl)-
常見問題列表
生物活性
R916562 是口服有效的，選擇性的 Axl/VEGF-R2 雙抑制劑，IC50 分別為 136 nM 和 24 nM。R916562 具有抗血管生成和抗癌轉(zhuǎn)移作用。靶點
|
VEGF-R2 24 nM (IC 50 ) |
Axl 136 nM (IC 50 ) |
體內(nèi)研究
R916562 treatment at 85 mg/kg or 125 mg/kg orally b.i. d for 21 days results in statistically significant tumor growth inhibitions of 69% or 83% respectively. R916562 shows 73% reduction in fibroblast growth factor-induced neovascularization in a mouse corneal micropocket assay at a dose of 100 mg/kg and 50% reduction at 50 mg/kg.